Phosphodiesterase (PDE)
Phosphodiesterase (PDE) is any enzyme that breaks a phosphodiester bond. Usually, people speaking of phosphodiesterase are referring to cyclic nucleotide phosphodiesterases, which have great clinical significance and are described below. However, there are many other families of phosphodiesterases, including phospholipases C and D, autotaxin, sphingomyelin phosphodiesterase, DNases, RNases, and restriction endonucleases, as well as numerous less-well-characterized small-molecule phosphodiesterases. The cyclic nucleotide phosphodiesterases comprise a group of enzymes that degrade the phosphodiester bond in the second messenger molecules cAMP and cGMP. They regulate the localization, duration, and amplitude of cyclic nucleotide signaling within subcellular domains. PDEs are therefore important regulators ofsignal transduction mediated by these second messenger molecules.
Phosphodiesterase (PDE) Isoform Specific Products
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Phosphodiesterase (PDE)
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PDE1
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PDE2
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PDE3
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PDE4
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PDE5
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PDE6
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PDE7
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PDE9
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PDE10
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PDE11
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PDE12
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PDE8
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Autotaxin
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All Product Categories
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Phosphodiesterase (PDE) Inhibitors
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Phosphodiesterase (PDE) Agonists
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Phosphodiesterase (PDE) Antagonists
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Phosphodiesterase (PDE) Activators
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Phosphodiesterase (PDE) Modulators
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Phosphodiesterase (PDE) Degraders
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Phosphodiesterase (PDE) Controls
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Phosphodiesterase (PDE) Substrates
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Phosphodiesterase (PDE) Ligand
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Phosphodiesterase (PDE) Related Products (1005)
Related Products (1005)
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Antibodies (4)
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Phosphodiesterase (PDE) Isoform Comparison
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Anagrelide
0 ImagesAnagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action.
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Dihydroergotoxine mesylate
0 ImagesDihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.Dihydroergotoxine mesylate (Ergoloid mesylates) is an α-adrenergic blocking agent. Dihydroergotoxine mesylate binds with high affinity to the GABAA receptor associated Cl- channel. Dihydroergotoxine mesylate also interacts with central dopaminergic and serotonergic receptors. Dihydroergotoxine mesylate displays antiproliferative, antihypertensive and neuroprotective activity.
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Cilomilast
0 ImagesSynonyms: SB-207499Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 μM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
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PF-06445974
0 ImagesPF-06445974, a promising positron emission tomography (PET) lead, has exquisite potency at PDE4B with an IC50 <1 nM. The IC50 values are 36, 4.7 and 17 nM for PDE4D, PDE4A and PDE4C, respectively. PF-06445974 has good selectivity over PDE4D, excellent brain permeability, and a high level of specific binding in the "cold tracer" study.
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3-O-Methylquercetin
0 Images3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma.
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Tanimilast
0 ImagesSynonyms: CHF-6001Tanimilast (CHF-6001) is an orally active and selective phosphodiesterase 4 inhibitor (IC50=0.026 nM) with robust anti-inflammatory activity and suitable for topical pulmonary administration. Tanimilast increases cellular cAMP levels, and inhibits NF-κB signaling pathway. Tanimilast is used for the research of obstructive lung diseases.
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DNMDP
0 ImagesDNMDP, a phosphodiesterase 3A (PDE3A) inhibitor, is a potent and selective cancer cell cytotoxic agent. DNMDP binding to PDE3A promotes an interaction between PDE3A and Schlafen 12 (SLFN12). DNMDP shows clear cell-selective cytotoxicity.
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Theophylline (Standard)
0 ImagesSynonyms: 1,3-Dimethylxanthine(Standard); Theo-24 (Standard)Theophylline (Standard) is the analytical standard of Theophylline. This product is intended for research and analytical applications. Theophylline (1,3-Dimethylxanthine) is a potent phosphodiesterase (PDE) inhibitor, adenosine receptor antagonist, and histone deacetylase (HDAC) activator. Theophylline (1,3-Dimethylxanthine) inhibits PDE3 activity to relax airway smooth muscle. Theophylline (1,3-Dimethylxanthine) has anti-inflammatory activity by increase IL-10 and inhibit NF-κB into the nucleus. Theophylline (1,3-Dimethylxanthine) induces apoptosis. Theophylline (1,3-Dimethylxanthine) can be used for asthma and chronic obstructive pulmonary disease (COPD) research.
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Triflusal
0 ImagesTriflusal is an orally bioavailable, blood-brain barrier-permeable dual Cyclooxygenase-1 (COX-1)/cAMP phosphodiesterase inhibitor. Triflusal inhibits platelet aggregation, NF-κB activation, iNOS activity, and prostaglandin synthesis in ischaemic tissue. Triflusal stimulates neutrophil nitric oxide production, eNOS protein expression, and cNOS activity. Triflusal alleviates cerebral ischemic injury in rats and ameliorates pathological lesions and related gene expression in transgenic Alzheimer’s disease models. Triflusal can be used for the research of thromboembolic/ischemic cardiovascular and cerebrovascular diseases, and Alzheimer’s disease.
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ISM5939
0 ImagesISM5939 is an orally active and selective ENPP1 inhibitor with an IC50 of 0.63 nM for 2,3-cGAMP degradation and 9.28 nM for ATP hydrolysis. ISM5939 has antitumor activity.
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Doxofylline
0 ImagesDoxofylline is an orally active PDE IV inhibitor and A1AR antagonist. Doxofylline reduces inflammation in epithelial cells via inhibiting mitochondrial ROS production and amelioration of multiple cellular pathways (NLRP3-TXNIP inflammasome activation). Doxophylline can be used in studies of asthma, chronic obstructive pulmonary disease, and bronchospasm.
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Naperiglipron
0 ImagesSynonyms: LY3549492Naperiglipron (LY3549492) is an orally active Glucagon-like peptide 1 receptor (GLP-1R) agonist with an EC50 of 1.14 nM for hGLP-1R. Naperiglipron significantly decreases the level of blood glucose in GLP-1R knock-in mouse models. Naperiglipron inhibits PDE10A1 enzyme activity (IC50: 7.43 μM) with a weak hERG inhibitory activity. Naperiglipron can be used for type II diabetes mellitus (T2DM) and obesity research.
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Reproterol
0 ImagesReproterol is a selective β2-adrenoceptor agonist and cAMP phosphodiesterase (PDE) inhibitor. Reproterol inhibits adenylate cyclase-induced phosphodiesterase activity. Reproterol inhibits histamine release from mast cells. Reproterol is applicable to research related to asthma.
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Etazolate hydrochloride
0 ImagesSynonyms: SQ 20009; EHT 0202 hydrochlorideEtazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects.
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OPB-171775
0 ImagesOPB-171775 is an orally active molecular glue. OPB-171775 forms ternary complex with phosphodiesterase 3A (PDE3A) and schlafen family member 12 (SLFN12). OPB-171775 causes SLFN12 RNase-mediated cell death, activates SLFN12 RNase-associated GCN2 signaling pathway. OPB-171775 exhibits significant efficacy against gastrointestinal stromal tumor.
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Enpp-1-IN-12
0 ImagesEnpp-1-IN-12 (compound 43) is a potent and orally active ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor, with a Ki of 41 nM. Enpp-1-IN-12 exhibits anti-tumor activity.
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Enpp-1-IN-2
0 ImagesEnpp-1-IN-2 (Compound C) is a potent ENPP1 (ectonucleotide pyrophosphatase/phosphodiesterase 1) inhibitor with IC50 values of 0.26, 0.48 and 2.0 μM evaluated by means of TG-mAMP, pNP-TMP, and ATP assays, respectively. TG (Tokyo Green)-mAMP: a newly synthesized sensitive ENPP1 fluorescence probe.
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NPD-001
0 ImagesNPD-001 is a potent Trypanosoma brucei phosphodiesterases 1/2 (TbrPDEB1/2) inhibitor, with IC50 values of 4 and 3 nM, respectively. NPD-001 also inhibits hPDE4. NPD-001 can increase cAMP levels in parasites, prevent cytokinesis, and cause the parasites to form multinucleated, multi-flagellated cells that eventually lyse. NPD-001 can be used for the research of infection.
